AU2003271740B2 - Pseudopolymorphic forms of a HIV protease inhibitor - Google Patents

Pseudopolymorphic forms of a HIV protease inhibitor Download PDF

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Publication number
AU2003271740B2
AU2003271740B2 AU2003271740A AU2003271740A AU2003271740B2 AU 2003271740 B2 AU2003271740 B2 AU 2003271740B2 AU 2003271740 A AU2003271740 A AU 2003271740A AU 2003271740 A AU2003271740 A AU 2003271740A AU 2003271740 B2 AU2003271740 B2 AU 2003271740B2
Authority
AU
Australia
Prior art keywords
pseudopolymorph
compound
water
ethanol
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Revoked
Application number
AU2003271740A
Other languages
English (en)
Other versions
AU2003271740A1 (en
Inventor
Luc Donne Marie-Louise Janssens
Daniel Joseph Christiaan Thone
Hans Wim Pieter Vermeersch
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen R&D Ireland ULC
Original Assignee
Janssen R&D Ireland ULC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=29724454&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2003271740(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen R&D Ireland ULC filed Critical Janssen R&D Ireland ULC
Publication of AU2003271740A1 publication Critical patent/AU2003271740A1/en
Application granted granted Critical
Publication of AU2003271740B2 publication Critical patent/AU2003271740B2/en
Assigned to JANSSEN R&D IRELAND reassignment JANSSEN R&D IRELAND Request to Amend Deed and Register Assignors: TIBOTEC PHARMACEUTICALS LTD.
Anticipated expiration legal-status Critical
Revoked legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2003271740A 2002-05-16 2003-05-16 Pseudopolymorphic forms of a HIV protease inhibitor Revoked AU2003271740B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP02076929.5 2002-05-16
EP02076929 2002-05-16
PCT/EP2003/050176 WO2003106461A2 (en) 2002-05-16 2003-05-16 Pseudopolymorphic forms of a hiv protease inhibitor

Publications (2)

Publication Number Publication Date
AU2003271740A1 AU2003271740A1 (en) 2003-12-31
AU2003271740B2 true AU2003271740B2 (en) 2010-05-13

Family

ID=29724454

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2003271740A Revoked AU2003271740B2 (en) 2002-05-16 2003-05-16 Pseudopolymorphic forms of a HIV protease inhibitor
AU2012205289A Pending AU2012205289A1 (en) 2002-05-16 2012-07-03 Pseudopolymorphic forms of a HIV protease inhibitor

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2012205289A Pending AU2012205289A1 (en) 2002-05-16 2012-07-03 Pseudopolymorphic forms of a HIV protease inhibitor

Country Status (25)

Country Link
US (8) US7700645B2 (da)
EP (4) EP2314591B2 (da)
JP (1) JP4864320B2 (da)
KR (2) KR20100119906A (da)
CN (1) CN100475819C (da)
AP (1) AP2052A (da)
AU (2) AU2003271740B2 (da)
BR (1) BRPI0311176B8 (da)
CA (1) CA2485834C (da)
CY (3) CY1117928T1 (da)
DK (3) DK2767539T3 (da)
EA (1) EA007120B8 (da)
ES (4) ES2503551T5 (da)
HR (1) HRP20041061B1 (da)
HU (1) HUE034389T2 (da)
IL (1) IL165140A0 (da)
LT (1) LT2767539T (da)
MX (1) MXPA04011427A (da)
NO (1) NO331477B1 (da)
NZ (1) NZ536497A (da)
PL (1) PL215151B1 (da)
PT (3) PT2314591E (da)
SI (3) SI1567529T2 (da)
WO (1) WO2003106461A2 (da)
ZA (1) ZA200410154B (da)

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JP4776775B2 (ja) 1998-06-23 2011-09-21 アメリカ合衆国 Ｈｉｖ感染哺乳動物を治療するための医薬組成物
ES2503551T5 (es) 2002-05-16 2021-10-28 Janssen Sciences Ireland Unlimited Co Formas pseudopolimórficas de un inhibidor de la proteasa de VIH
HRP20020614A2 (en) * 2002-07-22 2004-06-30 PLIVA-ISTRAŽIVAČKI INSTITUT d.o.o. Rhombic pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin a
RS51073B (sr) 2003-12-23 2010-10-31 Tibotec Pharmaceuticals Ltd. Proces za pripremanje (3r,3as,6ar)-heksahidrofuro│2,3-b│ furan-3-il (1s,2r)-3-││(4-aminofenil) sulfonil│(izobutil) amino │-1-benzil-2-hidroksipropilkarbamata
AU2006217922B2 (en) 2005-02-25 2012-04-05 Janssen Sciences Ireland Uc Protease inhibitor precursor synthesis
ES2359949T3 (es) * 2006-11-09 2011-05-30 Tibotec Pharmaceuticals Métodos para preparar hexhidrofuro(2,3-b)furan-3-ol.
AR073248A1 (es) 2008-09-01 2010-10-20 Tibotec Pharm Ltd Proceso para la preparacion de (1s, 2r)-3- ((4-aminofenil) sulfonil) ( isobutil) amino)-1- bencil-2- hidroxipropilcarbamato de (3r, 3as,6ar)- hexahidrofuro-(2,3-b) furan-3- ilo (darunavir) y compuestos intermediarios utiles en dicho proceso.
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
US20120035142A1 (en) * 2009-01-29 2012-02-09 Mapi Pharma Limited Polymorphs of darunavir
WO2011048604A2 (en) * 2009-09-17 2011-04-28 Matrix Laboratories Limited An improved process for the preparation of darunavir
WO2011051978A2 (en) 2009-10-30 2011-05-05 Lupin Limited A novel process for preparation of darunavir and darunavir ethanolate of fine particle size
ES2546866T3 (es) * 2009-12-16 2015-09-29 Hetero Research Foundation Polimorfos de darunavir
AU2010340799B2 (en) * 2010-01-05 2015-06-11 Cipla Limited Darunavir polymorph and process for preparation thereof
EP2528923B1 (en) 2010-01-28 2014-07-30 Mapi Pharma Limited Process for the preparation of darunavir and darunavir intermediates
EP2571355B1 (en) 2010-05-20 2016-09-07 Hetero Research Foundation Crystalline hydrochloride salt of darunavir
WO2012107889A1 (en) 2011-02-10 2012-08-16 Ranbaxy Laboratories Limited Process for the preparation of amorphous darunavir
SI2729130T1 (en) 2011-07-07 2018-03-30 Janssen Sciences Ireland Uc Combined formulations of darunavir
WO2013114382A1 (en) 2011-12-05 2013-08-08 Mylan Laboratories Ltd Crystalline darunavir
WO2013108105A2 (en) * 2012-01-18 2013-07-25 Aurobindo Pharma Limited Novel solvates of darunavir
CN103509031B (zh) * 2012-06-20 2016-04-27 上海迪赛诺药业有限公司 制备达芦那韦无定形物的方法
ES2848216T3 (es) * 2012-07-24 2021-08-05 Laurus Labs Ltd Un proceso para la preparación de Darunavir
WO2014068265A1 (en) 2012-10-29 2014-05-08 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
US9346820B2 (en) * 2013-09-11 2016-05-24 Purdue Research Foundation HIV-1 protease inhibitors having gem-di-fluoro bicyclic P2-ligands
WO2016092525A1 (en) * 2014-12-12 2016-06-16 Lupin Limited Darunavir n-propanol solvate and process for preparation thereof
WO2016092527A1 (en) * 2014-12-12 2016-06-16 Sun Pharmaceutical Industries Limited A process for the preparation of dolutegravir
PL3271347T3 (pl) * 2015-03-19 2022-11-21 Mycovia Pharmaceuticals, Inc. Związki przeciwgrzybicze i sposoby wytwarzania
US20190175511A1 (en) 2016-08-08 2019-06-13 Hetero Labs Limited A Multi-Class Anti-Retroviral Composition
US11045423B2 (en) 2016-08-08 2021-06-29 Hetero Labs Limited Anti-retroviral compositions
US10407438B2 (en) 2016-10-27 2019-09-10 Gilead Sciences, Inc. Crystalline forms of darunavir
CN108727401A (zh) * 2017-04-20 2018-11-02 盐城迪赛诺制药有限公司 达鲁那韦新晶型及其制备方法和应用
CN109053753A (zh) * 2018-08-05 2018-12-21 浙江大学 一种制备达卢那韦二水合物晶型的方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0715618A1 (en) * 1993-08-24 1996-06-12 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1999067417A2 (en) * 1998-06-23 1999-12-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Fitness assay and associated methods
US6248775B1 (en) * 1992-08-25 2001-06-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors

Family Cites Families (13)

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US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
JPH05230044A (ja) 1992-02-21 1993-09-07 Hoechst Japan Ltd ピレタニドの新規な結晶多形
CN1072215C (zh) * 1995-02-22 2001-10-03 赫彻斯特药品和化学品公司 无定形吡咯他尼、吡咯他尼多晶型物,其制备方法和用途
CO4940492A1 (es) * 1997-05-29 2000-07-24 Merck & Co Inc Inhibidor de proteasa de vih
GB9712253D0 (en) 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
US6287693B1 (en) * 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
GB9805898D0 (en) * 1998-03-20 1998-05-13 Glaxo Group Ltd Process for the sythesis of hiv protease inhibitors
GB9807354D0 (en) 1998-04-07 1998-06-03 Glaxo Group Ltd Antiviral compound
WO1999067254A2 (en) * 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof
WO2000029390A1 (en) 1998-11-19 2000-05-25 Du Pont Pharmaceuticals Company Crystalline (-)-6- chloro-4- cyclopropylethynyl- 4-trifluoromethyl- 3,4-dihydro- 2(1h)-quinazolinone
EP1159278B1 (en) 1999-02-12 2005-11-30 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
ES2503551T5 (es) 2002-05-16 2021-10-28 Janssen Sciences Ireland Unlimited Co Formas pseudopolimórficas de un inhibidor de la proteasa de VIH
AU2010340799B2 (en) * 2010-01-05 2015-06-11 Cipla Limited Darunavir polymorph and process for preparation thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6248775B1 (en) * 1992-08-25 2001-06-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
EP0715618A1 (en) * 1993-08-24 1996-06-12 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1999067417A2 (en) * 1998-06-23 1999-12-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Fitness assay and associated methods

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Ghosh, A. K. et al., Bioorganic and Chemistry Letters 1998 vol 8 pp 687-690 *

Also Published As

Publication number Publication date
NO331477B1 (no) 2012-01-16
HUE034389T2 (en) 2018-02-28
NO20045409L (no) 2004-12-10
AP2052A (en) 2009-10-05
EP3045460A1 (en) 2016-07-20
EA200401503A1 (ru) 2005-06-30
CA2485834A1 (en) 2003-12-24
SI2314591T2 (sl) 2021-08-31
US20050250845A1 (en) 2005-11-10
US10858369B2 (en) 2020-12-08
US8518987B2 (en) 2013-08-27
CY1115665T1 (el) 2017-01-25
KR20100119906A (ko) 2010-11-11
EA007120B1 (ru) 2006-06-30
SI1567529T1 (sl) 2014-11-28
AP2004003191A0 (en) 2004-12-31
LT2767539T (lt) 2017-09-25
IL165140A0 (en) 2005-12-18
EP2767539A1 (en) 2014-08-20
WO2003106461A3 (en) 2004-05-13
EP2314591B1 (en) 2014-06-18
PT2767539T (pt) 2017-08-28
ES2498370T5 (es) 2021-11-24
CY1117928T1 (el) 2017-05-17
EP1567529B2 (en) 2021-02-24
EP1567529B1 (en) 2014-06-18
ES2498370T3 (es) 2014-09-24
HK1081969A1 (en) 2006-05-26
PT2314591E (pt) 2014-09-19
US20100204316A1 (en) 2010-08-12
AU2012205289A1 (en) 2012-08-09
HRP20041061A2 (en) 2006-07-31
BR0311176A (pt) 2005-03-15
CA2485834C (en) 2007-07-17
US20130303790A1 (en) 2013-11-14
SI2314591T1 (sl) 2014-11-28
DK1567529T4 (da) 2021-05-10
EP3045460B1 (en) 2019-04-17
DK1567529T3 (da) 2014-09-15
PL215151B1 (pl) 2013-10-31
EP1567529A2 (en) 2005-08-31
KR101128370B1 (ko) 2012-04-23
WO2003106461A2 (en) 2003-12-24
BRPI0311176B8 (pt) 2021-05-25
PL374321A1 (en) 2005-10-17
NZ536497A (en) 2006-08-31
EP2314591A1 (en) 2011-04-27
KR20050008715A (ko) 2005-01-21
DK2314591T4 (da) 2021-05-10
BRPI0311176B1 (pt) 2019-08-20
DK2767539T3 (da) 2017-09-11
EP2314591B2 (en) 2021-02-24
ES2503551T5 (es) 2021-10-28
EA007120B8 (ru) 2012-03-30
US20150336980A1 (en) 2015-11-26
US10000504B2 (en) 2018-06-19
US20210179631A1 (en) 2021-06-17
ES2638412T3 (es) 2017-10-20
DK2314591T3 (da) 2014-09-22
US7700645B2 (en) 2010-04-20
CN1668623A (zh) 2005-09-14
PT1567529E (pt) 2014-09-09
CY1119311T1 (el) 2018-02-14
JP4864320B2 (ja) 2012-02-01
HRP20041061B1 (hr) 2015-02-27
US20180312517A1 (en) 2018-11-01
AU2003271740A1 (en) 2003-12-31
EP2767539B1 (en) 2017-07-12
SI2767539T1 (sl) 2017-10-30
US20140171499A1 (en) 2014-06-19
ZA200410154B (en) 2005-12-28
ES2728735T3 (es) 2019-10-28
SI1567529T2 (sl) 2021-08-31
CN100475819C (zh) 2009-04-08
US20170260196A1 (en) 2017-09-14
JP2005533068A (ja) 2005-11-04
ES2503551T3 (es) 2014-10-07
MXPA04011427A (es) 2005-02-17

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MAK Offer to surrender letters patent
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Effective date: 20120809